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Asaraldehyde
COX抑制剂,用作医药中间体,用于制备细辛脑
目录号: PC14175 纯度: ≥98%
CAS No. :4460-86-0
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中文名称
Asaraldehyde
中文别名
细辛醛;2,4,5-三甲氧基苯甲醛;2,4,5-三甲氧基苯;2,4,5-三甲氧苯醛;2,4,5-三甲氧苯甲醛;細辛醛;环孢素A;环胞霉素A
英文名称
Asaraldehyde
英文别名
2,4,5-Trimethoxybenzaldehyde;2,4,5-trimethyl ether;3,4,6-trimethoxybenzaldehyde;asaraldehyde;asaronaldehyde;asarylaldehyde;gazarin;2,4,5-Trimethoxybenz;2,4,5-Trihydroxybenzaldehyde triMethyl ether;2,4,5-Trimethoxy;2,4,5-trimethoxy-Benzaldehyde;2,4,5-tris-methoxy benzaldehyde;Azarylaldehyde;Benzaldehyde, 2,4,5-trimethoxy-;NDU8J2Q00D;2,4,5-Trimethoxy benzaldehyde;IAJBQAYHSQIQRE-UHFFFAOYSA-N;SMR000112148;Asaraldehyde (Asaronaldehyde);Acrolein(Propenal);Pu
Cas No.
4460-86-0
分子式
C10H12O4
分子量
196.20
包装储存

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

生物活性

Asarylaldehyde (Asaronaldehyde), a COX-2 inhibitor, significantly inhibits cyclooxygenase II (COX-2) activity with an IC50 value of 100 μg/mL.

性状

Solid

IC50 & Target[1][2]

COX-2

 

体外研究(In Vitro)

Asarylaldehyde (2,4,5-TMBA) is a natural COX-2 inhibitor, which isolated from carrot (Daucus carota L.) seeds significantly inhibits cyclooxygenase II (COX-2) activity at the concentration of 100 μg/mL compared to three commercial nonsteroidal anti-inflammatory drugs Aspinin, Ibuprofen, and Naproxen at their IC50 values 180, 2.52, and 2.06 μg/mL, respectively. 2,4,5-TMBA, a natural inhibitor of cyclooxygenase-2, suppresses adipogenesis and oromotes lipolysis in 3T3-L1 adipocytes. 2,4,5-Trimethoxybenzaldehyde (2,4,5-TMBA) present in plant roots, seeds, and leaves is reported to be a significant inhibitor of cyclooxygenase-2 (COX-2) activity at the concentration of 100 μg/mL. Because COX-2 is associated with differentiation of preadipocytes, the murine 3T3-L1 cells are cultured with 100 μg/mL of 2,4,5-TMBA during differentiation and after the cells are fully differentiated to study the effect of 2,4,5-TMBA on adipogenesis and lipolysis. Oil Red O staining and triglyceride assay revealed that 2,4,5-TMBA inhibited the formation of lipid droplets during differentiation; moreover, 2,4,5-TMBA down-regulated the protein levels of adipogenic signaling molecules and transcription factors MAP kinase kinase (MEK), extracellular signal-regulated kinase (ERK), CCAAT/enhancer binding protein (C/EBP)α, β, and δ, peroxisome proliferator-activated receptor (PPAR)γ, adipocyte determination and differentiation-dependent factor 1 (ADD1), and the rate-limiting enzyme for lipid synthesis acetyl-CoA carboxylase (ACC). In fully differentiated adipocytes, treatment with 2,4,5-TMBA for 72 h significantly decreased lipid accumulation by increasing the hydrolysis of triglyceride through suppression of perilipin A (lipid droplet coating protein) and up-regulation of hormone-sensitive lipase (HSL). When treated with 100 μg/mL of 2,4,5-TMBA for 24, 48, or 72 h, the viability of fully differentiated 3T3-L1 adipocytes is decreased by 8.35, 15.54, and 27.26%, respectively. When the preadiocytes are treated with 100 μg/mL of 2,4,5-TMBA for 24 h before differentiation medium is supplemented, the cell viability is decreased by 26.46%. A COX-2 inhibitor 2,4,5-trimethoxybenzaldehyde (TMBA) is found to be the most abundant constituent, but is totally absent in its cultured broth and its natural host, C. kanehirae wood. 2,4,5-trimethoxybenzaldehyde (TMBA) is the major constituent in fruiting bodies.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

结构分类
来源
参考文献
溶解度数据
体外研究: 

DMSO : 100 mg/mL (509.68 mM; Need ultrasonic)

Ethanol : 50 mg/mL (254.84 mM; Need ultrasonic)

H2O : 0.14 mg/mL (0.71 mM; Need ultrasonic)

配制储备溶液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 5.0968 mL 25.4842 mL 50.9684 mL
5 mM 1.0194 mL 5.0968 mL 10.1937 mL
10 mM 0.5097 mL 2.5484 mL 5.0968 mL
*

产品不同,其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液;配成溶液后,建议分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C 储存时,建议在 6 个月内使用,-20°C 储存时,建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    建议依照次序添加每种溶剂: 10% EtOH    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 3.75 mg/mL (19.11 mM); Clear solution

    此方案可获得 ≥ 3.75 mg/mL (19.11 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 37.5 mg/mL 的澄清 EtOH 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 2.

    建议依照次序添加每种溶剂: 10% EtOH    90% corn oil

    Solubility: ≥ 3.75 mg/mL (19.11 mM); Clear solution

    此方案可获得 ≥ 3.75 mg/mL (19.11 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 37.5 mg/mL 的澄清 EtOH 储备液加到 900 μL玉米油中,混合均匀。

  • 3.

    建议依照次序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (12.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (12.74 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH?O 中,得到澄清透明的生理盐水溶液
  • 4.

    建议依照次序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (12.74 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (12.74 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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